Fabrication and Characterization of Electrospun Nanofibers for the Modified Release of the Chronobiotic Hormone Melatonin

Curr Drug Deliv. 2019;16(1):79-85. doi: 10.2174/1567201815666180914095701.

Abstract

Objective: Aiming at the modified release of melatonin (MLT), electrospun-MLT loaded nanofibers, filled into hard gelatin and DRcapsTM capsules, were used as formulants.

Methods: Cellulose acetate, polyvinylpyrrolidinone and hydroxypropylmethylcellusose (HPMC 2910) were used for the preparation of the fiber matrices through electrospinning. The in vitro modified release profile of MLT from the fabricated matrices in gastrointestinal-like fluids was studied. At pH 1.2, the formulations CA1, CA2, PV1, HP1, HP2 and the composite formulations CAPV1-CAPV5 in hard gelatin capsules exhibited fast MLT release.

Results: In general, the same trend was observed at pH 6.8, with the exception of CAPV1 and CAPV2. These two composite formulations delivered 52.08% and 75.25% MLT, respectively at a slower pace (6 h) when encapsulated in DRcapsTM capsules. In all other cases, the release of MLT from DRcapsTM capsules filled with the MLT-loaded nanofibers reached 100% at 6h.

Conclusion: These findings suggest that the MLT-loaded nanofibrous mats developed in this study exhibit a promising profile for treating sleep dysfunctions.

Keywords: Electrospun nanofibers; capsules; melatonin; modified release; polymers; scanning electron microscopic images..

MeSH terms

  • Administration, Oral
  • Cellulose / analogs & derivatives
  • Cellulose / chemistry
  • Central Nervous System Depressants / pharmacology*
  • Central Nervous System Depressants / therapeutic use
  • Delayed-Action Preparations / pharmacology
  • Delayed-Action Preparations / therapeutic use
  • Drug Liberation*
  • Gelatin / chemistry
  • Hypromellose Derivatives / chemistry
  • Melatonin / pharmacology*
  • Melatonin / therapeutic use
  • Nanocapsules / chemistry*
  • Nanocomposites / chemistry
  • Povidone / chemistry
  • Sleep Wake Disorders / drug therapy

Substances

  • Central Nervous System Depressants
  • Delayed-Action Preparations
  • Nanocapsules
  • acetylcellulose
  • Hypromellose Derivatives
  • Gelatin
  • Cellulose
  • Povidone
  • Melatonin